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KI0776Azathioprine50 mg$154

Chemical Characteristic

Product NameAzathioprine
SynonymsImuran, BW 57-322
CAS No.446-86-6
Molecular Weight 277.26
FormulaC9H7N7O2S
Chemical Structure

Biological activities

Azathioprine is an immunosuppressant that is widely used for the prevention of rejection on organ transplantations, autoimmune diseases such as antoimmune hepatitis, rheumatic arthritis or chronic inflammatory bowel diseases. Azathioprine is a prodrug and it is bioactivated to 6-mercaptopurine (6-MP) through the reduction by glutathione (GSH). Azathioprine also inhibits the mixed lymphocyte reaction at concentrations of 1-10 µg/mL. In vitro generation of cytotoxic cells has been inhibited by azathioprine with an IC50 of 0.03 µg/mL.[1]Azathioprine dose-dependently suppresses peripheral blood mononuclear cell (PBMC) blastogenesis, with an IC50 of 230.4 nM.[2] Azathioprine inhibits the generation of T-cell-independent anti-DNP-AFC and cell-mediated immunity (CMI) with IC50 of 10 and 0.03 µg/mL, respectively. Besides, during the initial period of the responses, azathioprine can block both humoral and cellular immune responses. Azathioprine is capable of inhibiting T-cell-dependent immune responses and B-cell-dependent immune.[3] In vivo, azathioprine (50 mg/body weight) causes a severe oxidative insult in the liver.[4]

References

[1] Sugiyama K, et al. Comparison of suppressive potency between azathioprine and 6-mercaptopurine against mitogen-induced blastogenesis of human peripheral blood mononuclear cells in-vitro. J Pharm Pharmacol. 2003, 55 (3): 393-398. 閵嗏偓閵嗏偓
[2] Galanaud P, et al. Effect of azathioprine on in vitro antibody response. Differential effect on B cells involved in thymus-dependent and independent responses. Clin Exp Immunol. 1975, 22 (1): 139-152.
[3] Rollonghoff M, et al. Effect of azathioprine and cytosine arabinoside on humoral and cellular immunity in vitro. Clin Exp Immunol. 1973, 15 (2): 261-269.
[4] Shanmugarajan TS, et al. Ficus hispida Linn. Leaf extract possesses antioxidant potential and abrogates azathioprine induced prooxidant and antioxidant imbalance in rat liver. International Journal of Pharmacology. 2008, 4(5): 376-381.

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